Abstract
A series of pyridinium and phenyl carboxylate derivatives of 3-alkyl-N-hydroxysuccinimide has been synthesized; the compounds have been shown to be highly effective, time-dependent inactivators of human leukocyte elastase. The cationic inhibitor having an isobutyl side chain as the P1 residue (3) was found to be the most effective. Human leukocyte cathepsin G and chymotrypsin are also inactivated by these compounds.
Publication types
-
Research Support, U.S. Gov't, P.H.S.
MeSH terms
-
Benzoates / chemical synthesis
-
Benzoates / pharmacology*
-
Cathepsin G
-
Cathepsins / antagonists & inhibitors
-
Chemical Phenomena
-
Chemistry, Physical
-
Chymotrypsin / antagonists & inhibitors
-
Humans
-
In Vitro Techniques
-
Leukocytes / enzymology*
-
Magnetic Resonance Spectroscopy
-
Pancreatic Elastase / antagonists & inhibitors*
-
Pyridinium Compounds / chemical synthesis
-
Pyridinium Compounds / pharmacology*
-
Serine Endopeptidases
-
Succinimides / chemical synthesis
-
Succinimides / pharmacology*
Substances
-
Benzoates
-
Pyridinium Compounds
-
Succinimides
-
Cathepsins
-
Serine Endopeptidases
-
Chymotrypsin
-
CTSG protein, human
-
Cathepsin G
-
Pancreatic Elastase